WO1999043654A3 - Inhibitors of phospholipase enzymes - Google Patents

Inhibitors of phospholipase enzymes Download PDF

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Publication number
WO1999043654A3
WO1999043654A3 PCT/US1999/003898 US9903898W WO9943654A3 WO 1999043654 A3 WO1999043654 A3 WO 1999043654A3 US 9903898 W US9903898 W US 9903898W WO 9943654 A3 WO9943654 A3 WO 9943654A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
phospholipase enzymes
compounds
mammal
administration
Prior art date
Application number
PCT/US1999/003898
Other languages
French (fr)
Other versions
WO1999043654A2 (en
Inventor
Jasbir S Seehra
John C Mckew
Frank Lovering
Jean E Bemis
Yibin Xiang
Lihren Chen
John L Knopf
Original Assignee
Genetics Inst
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to NZ506329A priority Critical patent/NZ506329A/en
Priority to BR9908275-6A priority patent/BR9908275A/en
Priority to IL13771999A priority patent/IL137719A0/en
Priority to EP99908378A priority patent/EP1062205A2/en
Priority to JP2000533412A priority patent/JP2002504541A/en
Priority to EA200000871A priority patent/EA003876B1/en
Priority to KR1020007009457A priority patent/KR20010041344A/en
Priority to EEP200000488A priority patent/EE200000488A/en
Application filed by Genetics Inst filed Critical Genetics Inst
Priority to HU0101146A priority patent/HUP0101146A3/en
Priority to SK1275-2000A priority patent/SK12752000A3/en
Priority to AU27825/99A priority patent/AU765427B2/en
Priority to CA002322162A priority patent/CA2322162A1/en
Publication of WO1999043654A2 publication Critical patent/WO1999043654A2/en
Publication of WO1999043654A3 publication Critical patent/WO1999043654A3/en
Priority to NO20004219A priority patent/NO20004219L/en
Priority to HR20000551A priority patent/HRP20000551A2/en
Priority to BG104779A priority patent/BG104779A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Abstract

This invention concerns compounds and pharmaceutical compositions useful for treating or preventing inflammatory conditions in a mammal, the methods comprising administration of novel pharmaceutically useful compounds of general formulae (I) or (II) or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined in the specification.
PCT/US1999/003898 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes WO1999043654A2 (en)

Priority Applications (15)

Application Number Priority Date Filing Date Title
HU0101146A HUP0101146A3 (en) 1998-02-25 1999-02-24 Indole derivatives as inhibitors of phospholipase enzymes and pharmaceutical compositions containing them
BR9908275-6A BR9908275A (en) 1998-02-25 1999-02-24 Phospholipase enzyme inhibitors
SK1275-2000A SK12752000A3 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
JP2000533412A JP2002504541A (en) 1998-02-25 1999-02-24 Phospholipase enzyme inhibitor
EA200000871A EA003876B1 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
KR1020007009457A KR20010041344A (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
EEP200000488A EE200000488A (en) 1998-02-25 1999-02-24 Phospholipase enzyme inhibitors and pharmaceutical compositions
NZ506329A NZ506329A (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
IL13771999A IL137719A0 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
EP99908378A EP1062205A2 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
AU27825/99A AU765427B2 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
CA002322162A CA2322162A1 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes
NO20004219A NO20004219L (en) 1998-02-25 2000-08-23 Inhibitors of phospholipase enzymes
HR20000551A HRP20000551A2 (en) 1998-02-25 2000-08-24 Inhibitors of phospholipase enzymes
BG104779A BG104779A (en) 1998-02-25 2000-09-19 Inhibitors of phospholipase enzymes

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3059298A 1998-02-25 1998-02-25
US09/030,592 1998-02-25

Publications (2)

Publication Number Publication Date
WO1999043654A2 WO1999043654A2 (en) 1999-09-02
WO1999043654A3 true WO1999043654A3 (en) 1999-10-28

Family

ID=21854952

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1999/003898 WO1999043654A2 (en) 1998-02-25 1999-02-24 Inhibitors of phospholipase enzymes

Country Status (21)

Country Link
EP (1) EP1062205A2 (en)
JP (1) JP2002504541A (en)
KR (1) KR20010041344A (en)
CN (1) CN1310706A (en)
AU (1) AU765427B2 (en)
BG (1) BG104779A (en)
BR (1) BR9908275A (en)
CA (1) CA2322162A1 (en)
EA (1) EA003876B1 (en)
EE (1) EE200000488A (en)
GE (1) GEP20032920B (en)
HR (1) HRP20000551A2 (en)
HU (1) HUP0101146A3 (en)
ID (1) ID26250A (en)
IL (1) IL137719A0 (en)
NO (1) NO20004219L (en)
NZ (1) NZ506329A (en)
PL (1) PL343007A1 (en)
SK (1) SK12752000A3 (en)
TR (1) TR200002447T2 (en)
WO (1) WO1999043654A2 (en)

Cited By (9)

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US8865737B2 (en) 2006-08-28 2014-10-21 Eisai R&D Management Co., Ltd. Antitumor agent for undifferentiated gastric cancer
US8952035B2 (en) 2007-11-09 2015-02-10 Eisai R&D Management Co., Ltd. Combination of anti-angiogenic substance and anti-tumor platinum complex
US8962655B2 (en) 2007-01-29 2015-02-24 Eisai R&D Management Co., Ltd. Composition for treatment of undifferentiated gastric cancer
US8962650B2 (en) 2011-04-18 2015-02-24 Eisai R&D Management Co., Ltd. Therapeutic agent for tumor
US8969344B2 (en) 2005-08-02 2015-03-03 Eisai R&D Management Co., Ltd. Method for assay on the effect of vascularization inhibitor
US9006256B2 (en) 2006-05-18 2015-04-14 Eisai R&D Management Co., Ltd. Antitumor agent for thyroid cancer
US9012458B2 (en) 2010-06-25 2015-04-21 Eisai R&D Management Co., Ltd. Antitumor agent using compounds having kinase inhibitory effect in combination
US9334239B2 (en) 2012-12-21 2016-05-10 Eisai R&D Management Co., Ltd. Amorphous form of quinoline derivative, and method for producing same
US9504746B2 (en) 2004-09-17 2016-11-29 Eisai R&D Management Co., Ltd. Pharmaceutical compositions of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide

Families Citing this family (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19917504A1 (en) * 1999-04-17 2000-10-19 Dresden Arzneimittel New hydroxy-indole derivatives, useful in treatment of degenerative joint disease, viral and parasitic infections, bronchial, dermatological, neurodegenerative and prostate disorders, etc.
ID27153A (en) * 1998-05-01 2001-03-08 Lilly Co Eli SPLA2 INHIBITOR COMPOUNDS TO TREAT DISEASE
TWI269654B (en) * 1999-09-28 2007-01-01 Baxter Healthcare Sa N-substituted indole-3-glyoxylamide compounds having anti-tumor action
DE19951360A1 (en) * 1999-10-26 2001-05-03 Aventis Pharma Gmbh Substituted indoles
DE19962300A1 (en) * 1999-12-23 2001-06-28 Asta Medica Ag New N-benzylindolyl glyoxylic acid derivatives are useful as antitumor agents
DE19963178A1 (en) 1999-12-27 2001-07-05 Gruenenthal Gmbh Substituted indole Mannich bases
DE10006139A1 (en) * 2000-02-11 2001-08-16 Merck Patent Gmbh Indol-3-yl derivatives
AUPQ876400A0 (en) * 2000-07-14 2000-08-03 University Of Queensland, The Compositions and method of using them
AU2001277056B2 (en) * 2000-07-25 2005-09-29 Merck & Co., Inc. N-substituted indoles useful in the treatment of diabetes
DE10037310A1 (en) 2000-07-28 2002-02-07 Asta Medica Ag New indole derivatives and their use as medicines
ES2318649T3 (en) 2000-10-20 2009-05-01 EISAI R&D MANAGEMENT CO., LTD. PROCEDURE FOR PREPARATION OF DERIVATIVES OF 4-FENOXI QUINOLINAS.
EP1349858B1 (en) 2000-11-02 2008-08-27 THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES Agents useful for reducing amyloid precursor protein and treating demantia and methods of use thereof
EP1844771A3 (en) * 2001-06-20 2007-11-07 Wyeth Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
DK1397130T3 (en) 2001-06-20 2007-11-12 Wyeth Corp Substituted Indole Acid Derivatives as Inhibitors of Plasminogen Activator Inhibitor-1 (PAI-1)
TWI224101B (en) 2001-06-20 2004-11-21 Wyeth Corp Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
MXPA04001089A (en) 2001-08-03 2004-05-20 Upjohn Co 5-arylsulfonyl indoles having 5-ht6 receptor affinity.
JP2005504790A (en) 2001-09-13 2005-02-17 シンタ ファーマスーティカルズ コーポレイション 3-glyoxylylamidoindole for treating cancer
US6984735B2 (en) 2001-12-03 2006-01-10 Wyeth Process for making an aldehyde
US7101875B2 (en) 2001-12-03 2006-09-05 Wyeth Methods for treating arthritic disorders
ES2300490T3 (en) * 2001-12-03 2008-06-16 Wyeth CITOSOLICA A2 PHOSPHOLIPASE INHIBITORS.
US7713964B2 (en) 2001-12-03 2010-05-11 Wyeth Llc Methods for treating asthmatic conditions
US7605156B2 (en) 2001-12-03 2009-10-20 Wyeth Methods for the use of inhibitors of cytosolic phospholipase A2
US6797708B2 (en) 2001-12-03 2004-09-28 Wyeth Inhibitors of cytosolic phospholipase A2
US6635771B2 (en) 2001-12-03 2003-10-21 Wyeth N-benzhydryl indole compounds
EP1495016A2 (en) * 2002-04-09 2005-01-12 Astex Technology Limited Heterocyclic compounds and their use as modulators of p38 map kinase
AUPS282602A0 (en) 2002-06-07 2002-06-27 Garvan Institute Of Medical Research Method of inhibiting cell proliferation
JP4340232B2 (en) 2002-08-29 2009-10-07 メルク エンド カムパニー インコーポレーテッド Indoles having anti-diabetic activity
WO2004020409A1 (en) 2002-08-29 2004-03-11 Merck & Co., Inc. Indoles having anti-diabetic activity
DK1569900T3 (en) 2002-12-10 2006-10-23 Wyeth Corp Substituted 3-carbonyl-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
UA80453C2 (en) 2002-12-10 2007-09-25 Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1)
CN1726191A (en) 2002-12-10 2006-01-25 惠氏公司 Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
CN1723198A (en) * 2002-12-10 2006-01-18 惠氏公司 Aryl, aryloxy, and alkyloxy substituted 1h-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
EP1569899B1 (en) 2002-12-10 2006-06-28 Wyeth Substituted 3-alkyl- and 3-arylalkyl-1h-indol-1-yl-acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)
US7129264B2 (en) * 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
US7332521B2 (en) 2003-09-25 2008-02-19 Wyeth Substituted indoles
US7265148B2 (en) 2003-09-25 2007-09-04 Wyeth Substituted pyrrole-indoles
US7163954B2 (en) 2003-09-25 2007-01-16 Wyeth Substituted naphthyl benzothiophene acids
US7446201B2 (en) 2003-09-25 2008-11-04 Wyeth Substituted heteroaryl benzofuran acids
US7582773B2 (en) 2003-09-25 2009-09-01 Wyeth Substituted phenyl indoles
US7268159B2 (en) 2003-09-25 2007-09-11 Wyeth Substituted indoles
US7141592B2 (en) 2003-09-25 2006-11-28 Wyeth Substituted oxadiazolidinediones
US7411083B2 (en) 2003-09-25 2008-08-12 Wyeth Substituted acetic acid derivatives
US7351726B2 (en) 2003-09-25 2008-04-01 Wyeth Substituted oxadiazolidinediones
US7442805B2 (en) 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
US7342039B2 (en) 2003-09-25 2008-03-11 Wyeth Substituted indole oximes
US7420083B2 (en) 2003-09-25 2008-09-02 Wyeth Substituted aryloximes
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
GB0412769D0 (en) 2004-06-08 2004-07-07 Novartis Ag Organic compounds
AU2005254782A1 (en) 2004-06-18 2005-12-29 Biolipox Ab Indoles useful in the treatment of inflammation
MX2007002178A (en) 2004-08-23 2007-04-02 Wyeth Corp Oxazolo-naphthyl acids as plaminogen activator inhibtor type-1 (pai-1) modulators useful in the treatment of thrombosis and cardiovascular diseases.
DE602005026867D1 (en) 2005-01-19 2011-04-21 Biolipox Ab INFLAMMATORY INDOL DERIVATIVES
WO2007024294A2 (en) 2005-05-03 2007-03-01 Cgi Pharmaceuticals, Inc. Certain substituted ureas, as modulators of kinase activity
GT200600228A (en) * 2005-05-27 2006-12-26 INHIBITORS OF PHOSPHOLIPASE A2 CITOSOLICA
AU2006279496A1 (en) 2005-08-17 2007-02-22 Wyeth Substituted indoles and use thereof
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US8410087B2 (en) * 2006-10-19 2013-04-02 Takeda Pharmaceutical Company Limited Indole compound
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ES2705950T3 (en) 2011-06-03 2019-03-27 Eisai R&D Man Co Ltd Biomarkers to predict and assess the responsiveness of subjects with thyroid and kidney cancer to lenvatinib compounds
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EP3860998B1 (en) 2018-10-05 2023-12-27 Annapurna Bio Inc. Compounds and compositions for treating conditions associated with apj receptor activity

Citations (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3271416A (en) * 1961-10-24 1966-09-06 Merck & Co Inc Indolyl aliphatic acids
FR1583552A (en) * 1967-04-11 1969-11-14
CH484111A (en) * 1966-04-12 1970-01-15 Sumitomo Chemical Co Process for preparing new derivatives of N-benzoyl-3-indolylic aliphatic acid
US3629284A (en) * 1965-04-19 1971-12-21 Sumitomo Chemical Co Process for the preparation of 3-indolyl aliphatic acid derivatives
FR2152377A1 (en) * 1971-09-09 1973-04-27 Sumitomo Chemical Co 1-phenyl-2-methyl-5-alkyl or alkoxy-3-indolylacetic acid - derivs - antiinflammatory, analgesic, antipyretic
FR2158464A1 (en) * 1971-11-03 1973-06-15 Ici Ltd
EP0337766A1 (en) * 1988-04-14 1989-10-18 Ici Americas Inc. Hetera-aliphatic carboxamides
EP0337767A1 (en) * 1988-04-13 1989-10-18 Ici Americas Inc. Cyclic amides
US4894386A (en) * 1987-04-15 1990-01-16 Ici Americas Inc. Aliphatic carboxamides
WO1992003132A1 (en) * 1990-08-20 1992-03-05 Abbott Laboratories Indole derivatives which inhibit leukotriene biosynthesis
EP0620214A1 (en) * 1993-04-16 1994-10-19 Eli Lilly And Company 1H-indole-3-acetic acid hydrazide sPLA2 inhibitors
EP0620215A1 (en) * 1993-04-16 1994-10-19 Eli Lilly And Company 1H-indole-3-acetamide derivatives as sPLA2 inhibitors
WO1995013266A1 (en) * 1993-11-12 1995-05-18 Merckle Gmbh Chem.-Pharm. Fabrik Acylpyrrole-alkanoic acids and indole-2-alkanoic acids plus their derivatives for use as inhibitors of phospholipase a¿2?
US5420289A (en) * 1989-10-27 1995-05-30 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
EP0675110A1 (en) * 1994-04-01 1995-10-04 Eli Lilly And Company 1H-Indole-3-glyoxylamide sPLA2 inhibitors
WO1996037467A1 (en) * 1995-05-22 1996-11-28 Merck Frosst Canada Inc. N-benzylindol-3-yl butanoic acid derivatives as cyclooxygenase-2 inhibitors
WO1996037469A1 (en) * 1995-05-22 1996-11-28 Merck Frosst Canada Inc. N-benzylindol-3-yl propanic acid derivatives as cyclooxygenase-2 inhibitors
WO1997013751A1 (en) * 1995-10-10 1997-04-17 Pfizer Inc. Indole carbamates as leukotriene antagonists
WO1998005637A1 (en) * 1996-08-01 1998-02-12 Merckle Gmbh Acylpyrroldicarboxylic acids and acylindoldicarboxylic acids and their derivatives and inhibitors of the cytosolic phospholipase a¿2?
WO1998008818A1 (en) * 1996-08-26 1998-03-05 Genetics Institute, Inc. Inhibitors of phospholipase enzymes

Patent Citations (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3271416A (en) * 1961-10-24 1966-09-06 Merck & Co Inc Indolyl aliphatic acids
US3629284A (en) * 1965-04-19 1971-12-21 Sumitomo Chemical Co Process for the preparation of 3-indolyl aliphatic acid derivatives
CH484111A (en) * 1966-04-12 1970-01-15 Sumitomo Chemical Co Process for preparing new derivatives of N-benzoyl-3-indolylic aliphatic acid
FR1583552A (en) * 1967-04-11 1969-11-14
FR2152377A1 (en) * 1971-09-09 1973-04-27 Sumitomo Chemical Co 1-phenyl-2-methyl-5-alkyl or alkoxy-3-indolylacetic acid - derivs - antiinflammatory, analgesic, antipyretic
FR2158464A1 (en) * 1971-11-03 1973-06-15 Ici Ltd
US4894386A (en) * 1987-04-15 1990-01-16 Ici Americas Inc. Aliphatic carboxamides
EP0337767A1 (en) * 1988-04-13 1989-10-18 Ici Americas Inc. Cyclic amides
EP0337766A1 (en) * 1988-04-14 1989-10-18 Ici Americas Inc. Hetera-aliphatic carboxamides
US5420289A (en) * 1989-10-27 1995-05-30 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
WO1992003132A1 (en) * 1990-08-20 1992-03-05 Abbott Laboratories Indole derivatives which inhibit leukotriene biosynthesis
EP0620214A1 (en) * 1993-04-16 1994-10-19 Eli Lilly And Company 1H-indole-3-acetic acid hydrazide sPLA2 inhibitors
EP0620215A1 (en) * 1993-04-16 1994-10-19 Eli Lilly And Company 1H-indole-3-acetamide derivatives as sPLA2 inhibitors
WO1995013266A1 (en) * 1993-11-12 1995-05-18 Merckle Gmbh Chem.-Pharm. Fabrik Acylpyrrole-alkanoic acids and indole-2-alkanoic acids plus their derivatives for use as inhibitors of phospholipase a¿2?
EP0675110A1 (en) * 1994-04-01 1995-10-04 Eli Lilly And Company 1H-Indole-3-glyoxylamide sPLA2 inhibitors
WO1996037467A1 (en) * 1995-05-22 1996-11-28 Merck Frosst Canada Inc. N-benzylindol-3-yl butanoic acid derivatives as cyclooxygenase-2 inhibitors
WO1996037469A1 (en) * 1995-05-22 1996-11-28 Merck Frosst Canada Inc. N-benzylindol-3-yl propanic acid derivatives as cyclooxygenase-2 inhibitors
WO1997013751A1 (en) * 1995-10-10 1997-04-17 Pfizer Inc. Indole carbamates as leukotriene antagonists
WO1998005637A1 (en) * 1996-08-01 1998-02-12 Merckle Gmbh Acylpyrroldicarboxylic acids and acylindoldicarboxylic acids and their derivatives and inhibitors of the cytosolic phospholipase a¿2?
WO1998008818A1 (en) * 1996-08-26 1998-03-05 Genetics Institute, Inc. Inhibitors of phospholipase enzymes

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, vol. 121, no. 11, 12 September 1994, Columbus, Ohio, US; abstract no. 124872, XP002114445 *
CHEMICAL ABSTRACTS, vol. 76, no. 5, 31 January 1972, Columbus, Ohio, US; abstract no. 25103, XP002114446 *
CHEN, SI-FENG ET AL, ZHONGGUO YAOLI XUEBAO, vol. 15, no. 4, 1994, pages 299 - 302 *
R.D. DILLARD ET AL., JOURNAL OF MEDICINAL CHEMISTRY, vol. 39, 1996, WASHINGTON US, pages 5137 - 5158, XP002046055 *

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9504746B2 (en) 2004-09-17 2016-11-29 Eisai R&D Management Co., Ltd. Pharmaceutical compositions of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide
US8969344B2 (en) 2005-08-02 2015-03-03 Eisai R&D Management Co., Ltd. Method for assay on the effect of vascularization inhibitor
US9006240B2 (en) 2005-08-02 2015-04-14 Eisai R&D Management Co., Ltd. Method for assay on the effect of vascularization inhibitor
US9006256B2 (en) 2006-05-18 2015-04-14 Eisai R&D Management Co., Ltd. Antitumor agent for thyroid cancer
US8865737B2 (en) 2006-08-28 2014-10-21 Eisai R&D Management Co., Ltd. Antitumor agent for undifferentiated gastric cancer
US8962655B2 (en) 2007-01-29 2015-02-24 Eisai R&D Management Co., Ltd. Composition for treatment of undifferentiated gastric cancer
US8952035B2 (en) 2007-11-09 2015-02-10 Eisai R&D Management Co., Ltd. Combination of anti-angiogenic substance and anti-tumor platinum complex
US9012458B2 (en) 2010-06-25 2015-04-21 Eisai R&D Management Co., Ltd. Antitumor agent using compounds having kinase inhibitory effect in combination
US8962650B2 (en) 2011-04-18 2015-02-24 Eisai R&D Management Co., Ltd. Therapeutic agent for tumor
US9334239B2 (en) 2012-12-21 2016-05-10 Eisai R&D Management Co., Ltd. Amorphous form of quinoline derivative, and method for producing same

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